| Determining key compound
properties by experimental assays
The most important things that pharmaceutical companies need to
know about new compounds include their solubility, lipophilicity,
plasma proten binding and how they are metabolized by the liver.
For orally-administered compounds, drug researchers need a measure
of gastro-intestinal permeability. Cyprotex can provide a quality-assured
technology platform for the evaluation of all of these properties.
As compounds advance through the drug development process their
numbers decrease and the level of detail and accuracy needed in
evaluating relevant pharmacokinetic properties becomes necessarily
greater. Therefore, different methods for pharmacokinetic assessment
are employed depending on the stage the compound has reached in
the drug development process. Cyprotex has developed a range of
assays from high capacity in vitro ADME screening analyses for early
discovery projects through to the hand-crafted methods which are
necessary at the preclinical stages.
Cloe® Screen microsomal stability - evaluating thousands
of compounds reliably and cost-effectively
This assay gives an indication of a compound's potential to be
metabolized by the liver and hence whether it will reside in the
body long enough to have a sufficient therapeutic effect. It can
be easily adapted to investigate potential adverse drug response
resulting from drug-drug interactions. The assay measures how quickly
the compound disappears when placed in an environment that mimics
the model species liver. At Cyprotex, we follow the disappearance
of the test substance with liver microsomes - subcellular fractions
from liver cells that contain the major liver enzymes involved in
compound clearance or by using complete hepatocytes for more accurate,
hand-crafted evaluation for a handful of compounds. We are able
to generate intrinsic clearance results for both human and rat.
|